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NRX-252114

Chemical Structure : NRX-252114

CAS No.: 2763260-39-3

NRX-252114 (NRX 252114;NRX252114)

Catalog No.: PC-36151Not For Human Use, Lab Use Only.

NRX-252114 (NRX 252114, NRX252114) is a potent, small molecule β-TrCP-based degrader of β-catenin, potentiates pSer33/S37A β-catenin binding and ubiquitylation (EC50=6.5 nM).

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Biological Activity

NRX-252114 (NRX 252114, NRX252114) is a potent, small molecule β-TrCP-based degrader of β-catenin, potentiates pSer33/S37A β-catenin binding and ubiquitylation (EC50=6.5 nM).
NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with >1500-fold cooperativity, surpassing the affinity of WT doublyphosphorylated peptide in vitro, induces the degradation of an engineered mutant β-Catenin in a cellular system; inserts into a naturally occurring PPI interface, with contacts optimized for both the substrate and ligase within the same small molecule entity, which is distinct from PROTACs.

Physicochemical Properties

M.Wt 510.312
Formula C22H12Cl2F3N3O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(4-((2,6-dichlorophenyl)thio)-2-oxo-6-(trifluoromethyl)-1,2-dihydropyridine-3-carbonyl)isoindoline-4-carbonitrile

References

1. Simonetta KR, et al. Nat Commun. 2019 Mar 29;10(1):1402.

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